Therapeutically active compound and its use
    3.
    发明授权
    Therapeutically active compound and its use 失效
    治疗活性化合物及其用途

    公开(公告)号:US5124441A

    公开(公告)日:1992-06-23

    申请号:US728392

    申请日:1985-04-29

    摘要: Therapeutically active organic compound exhibiting at least one group comprising a structure --S'--S"--R, wherein the group --S"--R is defined by R being an organic group comprised in a physiologically acceptable compound H--S"--R obtainable by the splitting of the disulfide bridge --S'--S"-- in said structure, in which compound H--S"--R the sulfur atom S" is bound to a carbon atom in a heterocyclic aromatic ring in R having a configuration being such that the compound H--S"--R, while maintaining physiological acceptability, is stabilized, by tautomerism or resonance involving the sulfur atom S" bound to R, so as to be mainly excluded from reaction involving thiol disulfide exchange; S' being bound to an aliphatic carbon atom; and said compound, in addition to the group or groups comprising the structure --S'--S"--R, consisting of a residue of a therapeutically active organic base compound of non-polypeptide structure bound to S'.The invention also relates to a method of modifying a therapeutically active organic compound of non-polypeptide structure by introducing a structure --S'--S"--R according to above; a method of treating diseases by administration of a compound according to the invention and also to a pharmaceutical composition containing at least one compound according to the invention.

    摘要翻译: 表现出至少一个包含结构-S'-S“-R的基团的治疗活性有机化合物,其中基团-S”-R由R是由生理上可接受的化合物H-S“ -R可以通过在所述结构中分解二硫键-S'-S'而得到,其中化合物H-S“-R是硫原子S”与杂环芳环中的碳原子结合 R具有使得化合物H-S“-R'同时保持生理可接受性的稳定性,通过涉及与R结合的硫原子S”的互变异构体或共振,从而主要排除在涉及硫醇的反应之外 二硫化物交换; S'与脂肪族碳原子结合; 和所述化合物,除了包含结构-S'-S“-R”的基团或基团,由与S'结合的非多肽结构的治疗活性有机碱性化合物的残基组成。 本发明还涉及通过引入上述结构-S'-S“-R修饰非多肽结构的治疗活性有机化合物的方法; 通过施用根据本发明的化合物治疗疾病的方法,还涉及含有至少一种本发明化合物的药物组合物。